公开(公告)号：US20130252944A1

公开(公告)日：2013-09-26

申请号：US13809583

申请日：2011-07-11

申请人： Christelle Bolea ,  Sylvain Celanire ,  Lam Tang ,  Philip Jones ,  Nigel J. Liverton ,  Richard Soll ,  Jingchao Dong ,  Zhiyu Lei ,  Fuqing Liu ,  Yanling Kong ,  Yi Ju ,  Haoyong Zhang ,  Jieping Wei ,  Qiaoxin Wei ,  Minxiang Zhang ,  Yunfu Luo

发明人： Christelle Bolea ,  Sylvain Celanire ,  Lam Tang ,  Philip Jones ,  Nigel J. Liverton ,  Richard Soll ,  Jingchao Dong ,  Zhiyu Lei ,  Fuqing Liu ,  Yanling Kong ,  Yi Ju ,  Haoyong Zhang ,  Jieping Wei ,  Qiaoxin Wei ,  Minxiang Zhang ,  Yunfu Luo

IPC分类号： C07D513/04 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/506 ,  C07D513/14 ,  A61K45/06

CPC分类号： C07D513/12 ,  A23L27/2056 ,  A23L33/10 ,  A23V2002/00 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/06 ,  A61K9/10 ,  A61K9/2059 ,  A61K31/429 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/55 ,  A61K45/06 ,  C07D513/04 ,  C07D513/14 ,  A61K2300/00 ,  A23V2200/16 ,  A23V2200/322 ,  A23V2200/328

摘要： The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

摘要翻译： 本发明涉及新的式（I）化合物，其中M，A和Y如式（I）所定义; 本发明化合物是代谢型谷氨酸受体的调节剂 - 亚型4（“mGluR4”），其可用于治疗或预防中枢神经系统疾病以及由mGluR4受体调节的其它障碍。 本发明还涉及药物组合物和这些化合物在制备药物中的用途，以及这些化合物用于预防和治疗涉及mGluR4的疾病的用途。

公开(公告)号：US20140100231A1

公开(公告)日：2014-04-10

申请号：US14047515

申请日：2013-10-07

申请人： Kenneth L. Arrington ,  Christopher Burgey ,  Robert Gilfillan ,  Yongxin Han ,  Mehul Patel ,  Chun Sing Li ,  Yaozong Li ,  Yunfu Luo ,  Zhiyu Lei

发明人： Kenneth L. Arrington ,  Christopher Burgey ,  Robert Gilfillan ,  Yongxin Han ,  Mehul Patel ,  Chun Sing Li ,  Yaozong Li ,  Yunfu Luo ,  Zhiyu Lei

IPC分类号： A61K31/513 ,  C07D405/14 ,  C07D403/06 ,  C07D471/04 ,  A61K45/06

CPC分类号： C07D471/04 ,  A61K31/513 ,  A61K45/06 ,  C07D239/52 ,  C07D239/54 ,  C07D239/56 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14

摘要： Compounds of Formula I: are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

摘要翻译： 式I化合物是HIV逆转录酶抑制剂，其中R1，R2，RE，L，M和Z在本文中定义。 式I化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗HIV感染以及预防，延缓发作或进展以及AIDS治疗。 化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

公开(公告)号：US20230139282A1

公开(公告)日：2023-05-04

申请号：US17795349

申请日：2021-02-02

申请人： Manuel DE LERA RUIZ ,  Paola FAVUZZA ,  Zhuyan GUO ,  Bin HU ,  Michael J. KELLY, III ,  Zhiyu LEI ,  John A. MCCAULEY ,  David B. OLSEN ,  Brad SLEEBS ,  Tony TRIGLIA ,  Dongmei ZHAN ,  Lianyun ZHAO ,  Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R&D (China) Co., Ltd.

发明人： Manuel de Lera Ruiz ,  Paola Favuzza ,  Zhuyan Guo ,  Bin Hu ,  Michael J. Kelly, III ,  Zhiyu Lei ,  John A. McCauley ,  David B. Olsen ,  Brad Sleebs ,  Tony Triglia ,  Dongmei Zhan ,  Lianyun Zhao

IPC分类号： A61K31/513 ,  A61K45/06 ,  C07D405/12 ,  C07D233/88 ,  C07D405/14 ,  C07D417/14 ,  C07D491/18 ,  A61P33/06 ,  A61K31/529 ,  A61K31/5377 ,  C07D401/06

摘要： Provided are methods of treating malaria comprising administration of compounds of Formula (I) or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.